PBIT, JARID1 Histone Demethylases Inhibitor


Catalog No. size PriceQuantity
M60170-2S 2 mg solid $129
M60170-10S 10 mg solid $535

Description

Product Information
Molecular Weight: 241.31
Formula: C14H11NOS
Purity: ≥98%
CAS#: 2514-30-9
Solubility: DMSO up to 50 mM
Chemical Name: 2-4(4-methylphenyl)-1,2-benzisothiazol-3(2H)-one
Storage: Powder: 4oC 1 year. DMSO: 4oC 3 month; -20oC 1 year.

 

Biological Activity:

 

PBIT is a potent, specific, reversible and cell-permeable inhibitor of Jumonji AT-Rich Interactive Domain 1 (JARID1) histone demethylases. It inhibits JARID1B (also known as KDM5B or PLU1) with an IC₅₀ of ~3 μM in vitro. It also inhibits the activity of other related histone demethylases JARID1A, JARID1C, and JMJD2E with IC50 ~6, 4.9, and 28 µM respectively. PBIT does not affect the activity of unrelated UTX and JMJD3 H3K27me3 demethylases. HeLa cells overexpressing full length JARID1B showed a significant increase in H3K4Me3 level following PBIT treatment (~10 µM). It blocks the proliferation of UACC-812 tumor cells expressing higher levels of JARDID1B, but does not significantly affect MCF7 or MCF10A cells expressing lower levels of JARDID1B.

 


How to Use:

 

 

  • In vitro: PBIT was used at 10-30 µM in vitro.
  • In vivo: n/a

 

 

 


Reference:

 

  1. Sayegh J, et al. Identification of small molecule inhibitors of Jumonji AT-rich interactive domain 1B (JARID1B) histone demethylase by a sensitive high throughput screen. (2013) J Biol Chem. 288(13):9408-17.


 


Products are for research use only. Not for human use.

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